Yongjun Cheng1, Jingyi Zhu2, Lingzhou Zhao1, Zhijuan Xiong3, Yueqin Tang4, Changcun Liu1, Lilei Guo1, Wenli Qiao1, Xiangyang Shi2,3, Jinhua Zhao1. 1. Department of Nuclear Medicine, Shanghai General Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200080, People's Republic of China. 2. State Key Laboratory for Modification of Chemical Fibers & Polymer Materials, College of Materials Science & Engineering, Donghua University, Shanghai 201620, People's Republic of China. 3. College of Chemistry, Chemical Engineering & Biotechnology, Donghua University, Shanghai 201620, People's Republic of China. 4. Experiment Center, Shanghai General Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200080, People's Republic of China.
Abstract
AIM: The poly(amidoamine) dendrimers modified with Buthus martensii Karsch chlorotoxin (BmK CT) were developed as a (131)I delivery system for glioma-targeted imaging and therapy. MATERIALS & METHODS: Dendrimers before and after labeling (131)I were synthetized and their physicochemical properties were tested. The targeting and therapeutic efficacy of (131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer against glioma was evaluated in vitro and in vivo. RESULTS: All the dendrimers were stable under different conditions. BmK CT modification increased the cellular uptake of dendrimers in C6 glioma cells, but not in the normal RLE-6TN cells. (131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer was radiochemically pure and could be applied in glioma-targeting single-photon emission CT (SPECT) imaging and radiotherapy. CONCLUSION: (131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) complex is a promising multifunctional nanoplatform for glioma-specific nuclear imaging and radiotherapy.
AIM: The poly(amidoamine) dendrimers modified with Buthus martensii Karsch chlorotoxin (BmK CT) were developed as a (131)I delivery system for glioma-targeted imaging and therapy. MATERIALS & METHODS: Dendrimers before and after labeling (131)I were synthetized and their physicochemical properties were tested. The targeting and therapeutic efficacy of (131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer against glioma was evaluated in vitro and in vivo. RESULTS: All the dendrimers were stable under different conditions. BmK CT modification increased the cellular uptake of dendrimers in C6 glioma cells, but not in the normal RLE-6TN cells. (131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer was radiochemically pure and could be applied in glioma-targeting single-photon emission CT (SPECT) imaging and radiotherapy. CONCLUSION: (131)I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) complex is a promising multifunctional nanoplatform for glioma-specific nuclear imaging and radiotherapy.